Boneset
B
Summary and Pharmaceutical Comment
The constituents of boneset are fairly well documented and include many pharmacologically active classes such as flavonoids, sesquiterpene lactones (typical for the Asteraceae family) and triterpenes. Immunostimulant activity (in vitro) has been reported for sesquiterpene lactone and polysaccharide components, but there is a lack of rigorous clinical research assessing the efficacy of boneset. Many pharmacological studies have focused on the cytotoxic/ antitumour actions of sesquiterpene lactone components of various Eupatorium species, although these actions have not been reported for sesquiterpene lactones isolated from boneset. Little is known regarding the toxicity of boneset. Hepatotoxic pyrrolizidine alkaloids, which have been documented for other Eupatorium species, have not been reported for boneset.
Species (Family)
Eupatorium perfoliatum L. (Asteraceae/Compositae)
Synonym(s)
Common Boneset, Eupatorium chapmanii Small, Feverwort, Thoroughwort. Snakeroot has been used to describe poisonous
Eupatorium species.
Part(s) Used
Herb
Pharmacopoeial and Other Monographs
BHP 1983(G7)
Martindale 35th edition(G85)
Legal Category (Licensed Products)
GSL – as Boneset and Eupatorium.(G37)
Constituents
The following is compiled from several sources, including General References G22, G41 and G48.
Flavonoids Flavonol (kaempferol, quercetin) glycosides including astragalin, hyperoside and rutin; eupatorin (flavone) and dihydroflavonols.(1)
Terpenoids Sesquiterpene lactones including euperfolin and euperfolitin (germacranolides), eufoliatin (guianolide), eufoliatorin (dilactone guaiane) and euperfolide.(2) Sesquiterpenes, diterpenes (dendroidinic acid, hebeclinolide), triterpenes (a- amyrin, dotriacontane) and sterols (sitosterol, stigmasterol).
Other constituents Volatile oil, resin, wax, tannic and gallic acids, bitter glucoside, inulin, polysaccharides and sugars.
Food Use
Boneset is not used in foods.
Herbal Use
Boneset is stated to possess diaphoretic and aperient properties. Traditionally, it has been used for influenza, acute bronchitis, nasopharyngeal catarrh, and specifically for influenza with deep aching, and congestion of the respiratory mucosa.(G7, G64)
Dosage
Dosages for oral administration (adults) for traditional uses recommended in older standard herbal reference texts are given below.
Herb 1–2 g as an infusion three times daily.(G7)
Liquid extract 1–2 mL (1 : 1 in 25% alcohol) three times daily.(G7)
Tincture 1–4 mL (1 : 5 in 45% alcohol) three times daily.(G7)
Figure 1 Boneset (Eupatorium perfoliatum).
Figure 2 Boneset – dried drug substance (herb).
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Pharmacological Actions
In vitro and animal studies
Immunostimulant activity (in vitro stimulation of granulocyte phagocytic activity) has been demonstrated by high dilutions (10 5–10 7 g/100 mL) of various sesquiterpene lactones isolated from E. perfoliatum.(3) In addition, immunostimulating actions (granulocyte, macrophage and carbon clearance tests) have been documented for polysaccharide fractions from E. perfoliatum.(3, 4)
An ethanol extract of the whole plant has exhibited weak antiinflammatory activity in rats.(G41) Many activities, including antiinflammatory activity, have been documented for flavonoid compounds.
Clinical studies
None documented. Rigorous randomised controlled clinical trials assessing the effects of boneset are required.
Side-effects, Toxicity
Contact dermatitis has been reported for Eupatorium species, but not specifically for boneset (E. perfoliatum).(G51) Cytotoxic properties have been documented for a related species, E. cannabinum, and are attributed to the sesquiterpene lactone eupatoriopicrin. This compound has not been documented as a constituent of boneset. Hepatotoxic pyrrolizidine alkaloids (PAs) have been isolated from various Eupatorium species, although none have been documented as constituents of boneset (E. perfoliatum).(5)
Instances of allergic and anaphylactic reactions have been associated with the sesquiterpene lactone constituents in German chamomile, although no reactions specifically involving boneset have been documented.
The US Food and Drugs Administration (FDA) has classified boneset as a herb of undefined safety.(G22)
Boneset |
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Contra-indications, Warnings
The allergenic potential of sesquiterpene lactones is well |
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recognised. Individuals with a known hypersensitivity to other |
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members of the Asteraceae family (e.g. chamomile, feverfew, |
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ragwort, tansy) should avoid using boneset. Individuals with |
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existing hypersensitivities/allergies should use boneset with |
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caution. |
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Drug interactions None documented. However, the potential for |
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preparations of boneset to interact with other medicines |
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administered concurrently, particularly those with similar or |
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opposing effects, should be considered. |
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Pregnancy and lactation The safety of boneset taken during |
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pregnancy has not been established. In view of the lack of toxicity |
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data and the possibility of constituents with allergenic activity, the |
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use of boneset during pregnancy and lactation should be avoided. |
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Preparations |
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Proprietary multi-ingredient preparations |
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Australia: Flavons. UK: Catarrh Mixture. |
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References
1 Herz W et al. Dihydroflavonols and other flavonoids of Eupatorium species. Phytochemistry 1972; 11: 2859–2863.
2 Herz W et al. Sesquiterpene lactones of Eupatorium perfoliatum. J Org Chem 1977; 42: 2264–2271.
3Wagner H. Immunostimulants from medicinal plants. In: Chang HM et al, eds. Advances in Chinese Medicinal Materials Research.
Singapore: World Scientific, 1985: 159–170.
4 Wagner H et al. Immunostimulating polysaccharides (heteroglycans) of higher plants. Arzneimittelforschung 1985; 35: 1069.
5Pyrrolizidine Alkaloids. Environmental Health Criteria 80. Geneva: World Health Organization, 1988.
Borage
B
Summary and Pharmaceutical Comment
Limited information is available on the constituents of borage. No documented pharmacological data were located to support the traditional uses, although the mucilage content supports the use of borage as a demulcent. Interest has focused on the volatile oil as a source of gamolenic acid. Borage contains known toxic pyrrolizidine alkaloids, although at concentrations considerably lower than those found in comfrey for which human toxicity has been documented. However, it would seem wise to avoid excessive or prolonged ingestion of borage. It is unclear whether borage oil, currently available in food supplements, contains any pyrrolizidine alkaloids.
Species (Family)
Borago officinalis L. (Boraginaceae)
Synonym(s)
Beebread, Bee Plant, Burrage, Starflower (oil)
Part(s) Used
Herb
Pharmacopoeial and Other Monographs
BP 2007(G84)
Martindale 35th edition(G85)
Ph Eur 2007(G81)
Legal Category (Licensed Product)
Borage is not included in the GSL.(G37)
Constituents
The following is compiled from several sources, including General References G22 and G64.
Alkaloids Pyrrolizidine-type. Lycopsamine, intermedine, acetyllycopsamine, acetylintermedine, amabiline, supinine and thesinine (unsaturated).(1, 2) Concentrations reported as 0.01% and 2– 10 ppm for commercial dried samples. Alkaloid concentrations reportedly the same for fresh and dried samples; fresh samples revealed alkaloids as the free base in the roots and mainly as N- oxides in the leaves.
Mucilages 11.1%. Yielding glucose, galactose and arabinose.
Oil Rich in fatty acids, in particular gamolenic acid.
Other constituents Acids (acetic, lactic, malic, silicic), cyanogenetic compounds and tannins (up to 3%).
Food Use
Borage is occasionally used in salads and soups.
Herbal Use
Borage is stated to possess diaphoretic, expectorant, tonic, antiinflammatory and galactogogue properties.(3) Traditionally,
borage has been used to treat many ailments including fevers, coughs and depression.(3, G42, G64) Borage is also reputed to act as a
restorative agent on the adrenal cortex.(3) Borage oil (starflower oil) is used as an alternative source to evening primrose oil for gamolenic acid.
Figure 1 Selected constituents of borage. |
Figure 2 Borage (Borago officinalis). |
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Figure 3 Borage – dried drug substance (herb).
Dosage
Dosages for oral administration (adults) for traditional uses recommended in older and contemporary standard herbal reference texts are given below.
Infusion Two 5-mL spoonfuls of dried herb to one cup boiling water three times daily.(3)
Tincture 1–4 mL three times daily.(3)
Pharmacological Actions
In vitro and animal studies
Borage oil has been reported to attenuate cardiovascular reactivity to stress in rats.(4)
Clinical studies
The effect of borage seed oil on the cardiovascular reactivity of humans to acute stress has been studied in 10 individuals, who each received a total daily dose of 1.3 g for 28 days.(4) The individuals were required to undertake an acute psychological task requiring sensory intake and vigilance (Stroop colour test). Borage oil was found to attenuate cardiovascular reactivity to stress, indicated by a reduction in systolic blood pressure and heart rate and by increased task performance. The specific mechanisms by which borage exerts this effect were unknown, but a central mechanism of action of the fatty acids was suggested in view of the simultaneous reduction in heart rate and blood pressure.(4)
Borage |
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Side-effects, Toxicity
None documented. However, borage contains low concentrations |
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of unsaturated pyrrolizidine alkaloids, which are known to be |
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hepatotoxic in both animals and humans (see Comfrey).(5) |
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Contra-indications, Warnings |
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Evening primrose oil is recommended to be used with caution in |
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epileptic patients, especially in those with schizophrenia and/or |
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those taking phenothiazines (see Evening Primrose); on the basis |
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that borage oil, like evening primrose oil, also contains high |
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concentrations of gamolenic acid, borage oil should also be used |
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with caution in these patient groups. In view of the known toxic |
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pyrrolizidine alkaloid constituents, excessive or prolonged inges- |
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tion of borage should be avoided. In particular, infusions (e.g. |
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herbal teas) containing borage should be avoided. |
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Drug interactions |
None documented. However, the potential for |
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preparations of borage to interact with other medicines |
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administered concurrently, particularly those with similar or |
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opposing effects, should be considered. |
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Pregnancy and |
lactation |
In view of the documented |
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pyrrolizidine constituents and lack of toxicity data, borage should not be used during pregnancy or lactation.
Preparations
Proprietary single-ingredient preparations
Chile: Dexol.
Proprietary multi-ingredient preparations
Chile: Celltech Gold. Italy: Sclerovis H. New Zealand: Mr Nits. USA: Borage Oil; Omega-3 Complex; Omega-3 Glucosamine.
References
1Luthry J et al. Pyrrolizidin-Alkaloide in Arzneipflanzen der Boraginaceen: Borago officinalis and Pulmonaria officinalis. Pharm
Acta Helv 1984; 59: 242–246.
2 Larsen KM et al. Unsaturated pyrrolizidines from Borage (Borage officinalis) a common garden herb. J Nat Prod 1984; 47: 747–748.
3Hoffman D. The Herb Users Guide, the Basic Skills of Medical Herbalism. Wellingborough: Thorsons, 1987.
4Mills DE. Dietary fatty acid supplementation alters stress reactivity and performance in man. J Hum Hypertens 1989; 3: 111–116.
5Mattock AR. Chemistry and Toxicology of Pyrrolizidine Alkaloids. London: Academic Press, 1986.